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GSK-3 inhibitor 3

更新时间:2025-08-27 07:53:44

GSK-3 inhibitor 3结构式
GSK-3 inhibitor 3结构式
品牌特惠专场
常用名 GSK-3 inhibitor 3 英文名 GSK-3 inhibitor 3
CAS号 2227279-84-5 分子量 410.40
密度 N/A 沸点 N/A
分子式 C23H15FN6O 熔点 N/A
MSDS N/A 闪点 N/A

 GSK-3 inhibitor 3用途


GSK-3抑制剂3是GSK-3的选择性口服活性和脑渗透抑制剂,对GSK-3α和GSK-3β的IC50分别为0.35 nM和0.25 nM。GSK-3抑制剂3在三重转基因小鼠阿尔茨海默病模型中降低S396处的tau蛋白磷酸化水平,IC50为10nM。GSK-3抑制剂3可用于神经系统疾病研究[1]。

 GSK-3 inhibitor 3名称

英文名 GSK-3 inhibitor 3

 GSK-3 inhibitor 3生物活性

描述 GSK-3抑制剂3是GSK-3的选择性口服活性和脑渗透抑制剂,对GSK-3α和GSK-3β的IC50分别为0.35 nM和0.25 nM。GSK-3抑制剂3在三重转基因小鼠阿尔茨海默病模型中降低S396处的tau蛋白磷酸化水平,IC50为10nM。GSK-3抑制剂3可用于神经系统疾病研究[1]。
相关类别
靶点实验

GSK-3α:0.35 nM (IC50)

GSK-3β:0.25 nM (IC50)

CDK2:0.22 μM (IC50)

CDK5:1.3 μM (IC50)

体外研究 GSK-3抑制剂3(化合物34)(1μM)是 CDK2和 CDK5的高选择性抑制剂,对 CDK2和 CDK5的 IC50分别为 0.22微米和 1.3μM[1]
参考文献

[1]. Hartz RA, et.al. Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors. J Med Chem. 2023 Jun 8;66(11):7534-7552.  

 GSK-3 inhibitor 3物理化学性质

分子式 C23H15FN6O
分子量 410.40

 GSK-3 inhibitor 3靶点实验

查看更多实验

实验名称:Metabolic stability in mouse liver microsomes assessed as parent compound remaining a...
来源:ChEMBL
靶标:N/A
External Id:CHEMBL5343401
实验名称:Metabolic stability in human liver microsomes assessed as parent compound remaining a...
来源:ChEMBL
靶标:N/A
External Id:CHEMBL5343399
实验名称:Metabolic stability in rat liver microsomes assessed as parent compound remaining at ...
来源:ChEMBL
靶标:N/A
External Id:CHEMBL5343400
实验名称:Inhibition of GSK-3 in human U2OS cells transfected with beta-catenin GFP and 4R1N ta...
来源:ChEMBL
靶标:Glycogen synthase kinase-3 beta
External Id:CHEMBL5343398
实验名称:Displacement of FL-KRREILSRRP[ps]ERYR-NH2 from human recombinant N-terminal His6-tagg...
来源:ChEMBL
靶标:Glycogen synthase kinase-3 beta
External Id:CHEMBL5343395
实验名称:Displacement of FL-KRREILSRRP[ps]ERYR-NH2 from human recombinant full length GST-tagg...
来源:ChEMBL
靶标:Glycogen synthase kinase-3 alpha
External Id:CHEMBL5343396
实验名称:Permeability of the compound at 100 uM incubated for 4 hrs at pH 7.4 by PAMPA assay
来源:ChEMBL
靶标:N/A
External Id:CHEMBL5343445
实验名称:Ratio of drug concentration in brain to plasma in LaFerla 3x transgenic Alzheimer's d...
来源:ChEMBL
靶标:N/A
External Id:CHEMBL5343443
实验名称:Ratio of unbound drug concentration in mouse brain to plasma at 10 uM incubated for 5...
来源:ChEMBL
靶标:N/A
External Id:CHEMBL5343444
实验名称:Oral bioavailability in C57BL/6 mouse at 10 mg/kg by LC-MS/MS analysis
来源:ChEMBL
靶标:N/A
External Id:CHEMBL5343439
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